Key Pharmacological Details
Dabigatran etexilate is a prodrug that rapidly converts to its active form, dabigatran, which is the actual therapeutic agent. 1 This distinction is clinically important because:
Dabigatran itself is a highly polar molecule that cannot be absorbed from the gastrointestinal tract, necessitating the prodrug formulation for oral administration. 1
After oral absorption, dabigatran etexilate undergoes rapid ester cleavage by serine esterase enzymes (via two intermediates—BIBR 1087E and BIBR 951 CL) to produce the active dabigatran molecule. 1
The conversion process is independent of cytochrome P-450 enzymes, which significantly reduces the potential for drug-drug interactions compared to warfarin. 3
Mechanism of Action
Dabigatran functions as a selective, reversible, direct thrombin (factor IIa) inhibitor with a Ki of 4.5 ± 0.2 mM. 1 It works by:
Directly binding to the active site of thrombin through a salt bridge between its amidine group and Asp 189, along with hydrophobic interactions. 1
Acting as a univalent inhibitor that interacts only with the active site of thrombin, unlike hirudin derivatives that also bind to substrate recognition sites. 1
Clinical Nomenclature
In clinical practice and prescribing:
- The brand name is Pradaxa® 1, 4, 5
- The generic name is dabigatran etexilate 1, 2
- The active metabolite is simply called dabigatran 1, 3
When prescribing or documenting, use "dabigatran etexilate" as the generic name, though clinicians often refer to it simply as "dabigatran" in shorthand, understanding that the oral formulation is necessarily the etexilate prodrug. 2, 5